MDL-27048
MDL-27048, a tubulin inhibitor, binds competitively, reversibly to the Colchicine (HY-16569)-binding site on tubulin heterodimers. MDL-27048 inhibits microtubule assembly, induces slow depolymerization of preassembled microtubules, disrupts microtubule polymerization-depolymerization dynamics, and disrupts cytoplasmic microtubule networks. MDL-27048 exerts growth inhibitory effects on human cancer cells, induces mitotic arrest, and does not disrupt actin filaments at microtubule-depolymerizing concentrations. MDL-27048 can be used for the research of malignant tumors.
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- CAS. Nr.: 124711-23-5
- Formel: C20H23NO3
- Molecular Weight:325.40
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Speicherung:
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| K562 | IC50 |
0.012 μM
Compound: 3e
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Antiproliferative activity against human K562 cells after 5 days by MTT assay
Antiproliferative activity against human K562 cells after 5 days by MTT assay
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[PMID: 19837593] |
MDL-27048 (0.4-20 μM; 40 min, 25 °C) binds reversibly to one site per purified porcine brain tubulin heterodimer with an apparent equilibrium constant of (2.1-3.5) × 106 M-1, and its binding site overlaps with the podophyllotoxin/colchicine-binding site[2].
MDL-27048 (0.5-20 μM; 30-96 min) inhibits in vitro assembly of purified porcine brain tubulin into microtubules with an IC50 of 1 μM at 1 mg/mL tubulin, induces slow depolymerization of pre-assembled microtubules, and its inhibitory effect is reversible with taxol[2].
MDL-27048 (0.2-10 μM; 10 min-4 h, monitored 2-30 min after wash-off) induces concentration- and time-dependent reversible depolymerization of PtK2 cell cytoplasmic microtubules, with maximal depolymerization achieved at 2-5 μM for 3 h, and complete repolymerization within 15-30 min after drug removal[2].
MDL-27048 (0.05-1 μM; 3-27 h) induces mitotic arrest in SV40-3T3 cells, with significant arrest at 0.2 μM and a mitotic index increase to 12.7% at 1 μM after 9 h, causing accumulation of cells with doubled DNA content[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PtK2 cells
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Concentration:0.2 μM; 0.5 μM; 0.8 μM; 2 μM; 5 μM
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Incubation Time:3 h
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Result:Induced concentration-dependent depolymerization of cytoplasmic microtubules: 0.2 μM caused undulating peripheral microtubules; 0.5-1 μM caused partial depolymerization; 2-5 μM caused maximal depolymerization, leaving only a few drug-resistant microtubules per cell, with no effect on actin filaments.
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Cell Line:PtK2 cells
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Concentration:10 μM
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Incubation Time:10 min; 20 min; 80 min; 180 min
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Result:Caused full depolymerization within 3 h.
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Cell Line:SV40-3T3 cells
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Concentration:1 μM
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Incubation Time:3 h; 6 h; 9 h; 27 h
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Result:Increased the mitotic index from 1% (control) to 2.7% at 3 h, 10.2% at 6 h, and 12.7% at 9 h at 1 μM.
Caused a marked shift to higher DNA content in 1 μM-treated cells at 6-9 h, indicating accumulation of cells that completed S phase but failed to progress through mitosis.
Chemical Information
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CAS. Nr. 124711-23-5
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Molecular Weight 325.40
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Formel C20H23NO3
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SMILES
CN(C)C(C=C1)=CC=C1/C=C(C)/C(C2=C(C=CC(OC)=C2)OC)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Kim DY, et al. Design and biological evaluation of novel tubulin inhibitors as antimitotic agents using a pharmacophore binding model with tubulin. J Med Chem. 2006;49(19):5664-5670. [Content Brief]
[2]. Peyrot V, et al. Interaction of tubulin and cellular microtubules with the new antitumor drug MDL 27048. A powerful and reversible microtubule inhibitor. J Biol Chem. 1989 Dec 15;264(35):21296-301. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MDL-27048 Related Classifications
HY-182478 Related Classifications
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